A new synthetic approach for 8-deazafolic acid was devised beginning from 2-acetamide-4-hydroxy-6-formylpyrimidine and proceeding through 2-amino-4-hydroxy-6-formyl-1,3,5-triazanaphthalene as key intermediate. The process is also being extended to prepare 8=deazahomofolic acid. Other synthetic areas include 10-alkyl-10-deazaminopterins as extensions of previously reported lead, 10-deazaminopterin. These compounds approximate 10-deazaminopterin as inhibitors of DHFR from L. casei or L-1210. Growth inhibition of folate dependent organisms is also similar illustrating bulk tolerance in the bridge region. Examination of these analogs in experimental tumors in mice is now in progress. Preliminary synthetic approaches toward 5,10-dideazaminopterin and 5,10-methenyl-10-deazaminopterin are being carried out.